| A New Route for Synthesis of Entecavir |
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| 作者姓名： | Li Wei GUO Yuan Jing XIAO Li Ping YANG |
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| 作者单位： | Li Wei GUO，Yuan Jing XIAO，Li Ping YANG* Department of chemistry，East China Normal University，Shanghai 200062 |
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| 摘 要： | 2-Amino-1,9-dihydro-9-(1S,3R,4S)-4-hydroxy-3-(hydroxymethyl)-2-methylenecyclopen tyl]-6H-purin-6-one (entecavir, Scheme 1) is a novel carbocyclic 2-deoxyguanosine analog drug which has potent and selective anti hepatitis B virus (HBV) activity1-3. Entecavir is also effective against lamivudine-resistant YMDD mutants4. The US Food and Drug Administration (FDA) approved entecavir as a new preferred drug for the treatment of HBV after lamivudine in March, 2005. Scheme 1 The structure o…
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| 关 键 词： | 合成路线 Mitsunobu反应 改性 恩替卡韦 乙肝治疗 药物 |
| 收稿时间： | 2006-01-20 |
A New Route for Synthesis of Entecavir |
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| Li Wei GUO Yuan Jing XIAO Li Ping YANG.A New Route for Synthesis of Entecavir[J].Chinese Chemical Letters,2006,17(7):907-910. |
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| Authors: | Li Wei GUO Yuan Jing XIAO Li Ping YANG |
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| Abstract: | A new economical synthetic route of entecavir was presented,involving the preparation of the key intermediate 6. The synthesis of 6 was conveniently achieved in good overall yield by a modified Mitsunobu reaction. |
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| Keywords: | Entecavir new route synthesis |
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